The discovery of acylated β-amino acids as potent and orally bioavailable VLA-4 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 4, 2002, Pages 611-614

  Lin, Linus S ^a   Kopka, Ihor E ^a   Mumford, Richard A ^a   Magriotis, Plato A ^a   Lanza Jr , Thomas ^a   Durette, Philippe L ^a   Kamenecka, Theodore ^a   Young, David N ^a   Laszlo, Stephen E de ^a   McCauley, Ermenegilda ^a   Riper, Gail Van ^a   Kidambi, Usha ^a   Egger, Linda A ^a   Tong, Xinchun ^a   Lyons, Kathryn ^a   Vincent, Stella ^a   Stearns, Ralph ^a   Colletti, Adria ^a   Teffera, Yohannes ^a   Fenyk Melody, Judy ^a   Schmidt, John A ^a   MacCoss, Malcolm ^a   Hagmann, William K ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA AMINO ACID; BETA1 INTEGRIN; BLOCKING AGENT; CD29 ANTIGEN ANTAGONIST; UNCLASSIFIED DRUG; AMINO ACID; AUTACOID; VERY LATE ACTIVATION ANTIGEN 4;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTIGEN BINDING; ARTICLE; BIOAVAILABILITY; COMBINATORIAL CHEMISTRY; CONTROLLED STUDY; DRUG POTENCY; DRUG SPECIFICITY; MICROSOME; NONHUMAN; PLASMA PROTEIN BINDING; RAT; ACYLATION; ANIMAL; DRUG ANTAGONISM; DRUG SCREENING; METABOLIC CLEARANCE RATE; METABOLISM; ORAL DRUG ADMINISTRATION; PROTEIN BINDING; SPRAGUE DAWLEY RAT; STEREOISOMERISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ACYLATION; ADMINISTRATION, ORAL; AMINO ACIDS; ANIMALS; BIOLOGICAL AVAILABILITY; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG EVALUATION, PRECLINICAL; INFLAMMATION MEDIATORS; INTEGRIN ALPHA4BETA1; METABOLIC CLEARANCE RATE; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 18244374489     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(01)00818-6     Document Type: Article

References (20)